Biseptrim

Biseptrim is an antibacterial drug for systemic use. It contains a combination of sulfonamides and trimethoprim.

A complex bactericidal drug, which includes the element sulfamethoxazole (is a sulfanilamide with an average duration of action), which slows down the binding of vitamin B9 by developing competitive antagonism with PABA. The drug also includes the component trimethoprim, which slows down microbial dihydrofolate reductase, which is responsible for the processes of binding bioactive tetrahydrofolate. [ 1 ]

Indications Biseptrim

It is used in case of such violations:

• urinary tract infections associated with the action of drug-sensitive strains of Klebsiella, Morgan's bacteria, Escherichia coli, Proteus, Enterobacter and Proteus mirabilis;
• lesions in the digestive system associated with strains of Shigella Sonnei and Flexneri (bacterial shigellosis);
• toxoplasmosis;
• therapy and prevention of the development of pneumonia caused by the influence of pneumocystis carinii (diagnosed bacteriologically);
• active stage of chronic bronchitis (in adults) and otitis media (in children) associated with drug-sensitive pneumococci and Haemophilus influenzae;
• Traveler's diarrhea caused by E. coli.

Release form

The medicinal substance is released in the form of tablets - 10 pieces in a cell pack (there are 2 such packs in a box).

Pharmacodynamics

Co-trimoxazole demonstrates in vitro activity against Escherichia coli (including enteropathogenic strains), indole-positive Proteus strains (including common Proteus), Klebsiella, Pneumococcus, Morgan bacteria, Proteus mirabilis, Shigella Sonnei and Flexneri, Enterobacter and Influenza bacilli. [ 2 ]

The combination of elements, acting on one of the chains of biochemical transformations, causes a synergistic antibacterial effect and slows down the development of microbial resistance. [ 3 ]

Pharmacokinetics

Both components of the drug are absorbed into the blood from the gastrointestinal tract at a high rate. Serum Cmax values for both components are noted after 1-4 hours from the moment of oral administration. Synthesis with serum protein is 70% (trimethoprim) and 44-62% (sulfamethoxazole).

The distribution processes of each substance are different: the distribution of sulfamethoxazole occurs only in the extracellular environment, and that of trimethoprim occurs within all body fluids.

High values of trimethoprim are recorded in bronchial secretions, bile and prostate. The level of sulfamethoxazole in fluids is slightly lower. Both elements in high values are noted in sputum, middle ear fluid and vaginal secretions.

The distribution volume of sulfamethoxazole is 360 ml/kg; trimethoprim is 2 l/kg. Both elements participate in intrahepatic metabolic processes: sulfamethoxazole is acetylated and synthesized with glucuronic acid, and trimethoprim is oxidized and hydroxylated.

Excretion is mainly realized through the kidneys - by means of active secretion of tubules and filtration. The indicator of active substances in urine significantly exceeds blood values. In the period of 72 hours, 84.5% of sulfamethoxazole and 66.8% of trimethoprim are excreted with urine.

The half-life is 10 (sulfamethoxazole) and 8-10 hours (trimethoprim). In case of renal insufficiency, this indicator is prolonged for both substances.

Dosing and administration

The medicine should be taken orally, with or after food, with plain water.

Teenagers from 12 years old and adults.

For inflammation in the urinary tract, active stage of chronic bronchitis and digestive system infections associated with shigella, an average of 2 tablets should be taken twice a day.

In case of inflammation in the urinary tract, Biseptrim is used for 10-14 days, in case of gastrointestinal infections caused by Shigella - 5 days, in case of the active stage of chronic bronchitis - 2 weeks.

To treat traveler's diarrhea, take 2 tablets at 12-hour intervals until symptoms disappear.

For toxoplasmosis, the drug is taken according to the schemes described below:

• 2 tablets per day during the 1st week;
• 2 tablets per day (taken every other day, 3 times a week);
• 2 tablets 2 times a day (every other day, 3 times a week).

In case of bacteriologically diagnosed pneumonia caused by Pneumocystis carinii, 90-120 mg/kg of the medicine should be used per day (divided into equal 1-time portions). The tablets should be taken with 6-hour breaks for a period of 2-3 weeks. The same scheme is used for children aged 6-12 years.

To prevent the development of Pneumocystis pneumonia in people at risk, take 2 tablets once a day during the first week.

The daily serving size can be a maximum of 1920 mg (4 tablets).

For individuals with a CC level within 15-30 ml per minute, the dosage is reduced by half.

For children aged 6-12.

In the active stage of otitis media, inflammation of the urethra and gastrointestinal infection associated with the activity of shigella, use 1 tablet 2 times a day.

In case of inflammation of the urinary tract and otitis, the medicine is used for 10 days, and in case of infections in the gastrointestinal tract - 5 days.

• Application for children

The medicine in this form is not used in persons under 6 years of age.

Use Biseptrim during pregnancy

Biseptrim should not be prescribed during breastfeeding and pregnancy.

Contraindications

Main contraindications:

• severe intolerance to the components of the drug;
• liver/kidney failure (creatinine clearance below 15 ml per minute);
• anemia (megaloblastic, aplastic, folate deficiency and pernicious types);
• leukopenia and agranulocytosis;
• G6PD deficiency;
• BA;
• hyperbilirubinemia in children;
• diseases in the thyroid gland.

Side effects Biseptrim

Side effects include:

• disorders of the nervous system: dizziness and cephalgia. Possible development of depression, tremor, aseptic meningitis, apathy and peripheral neuritis;
• problems with the respiratory system: infiltrates inside the lungs, bronchial spasm;
• digestive disorders: vomiting, abdominal pain, loss of appetite and nausea, gastritis, stomatitis, diarrhea and glossitis. In addition, cholestasis, hepatitis, pseudomembranous enterocolitis, hepatonecrosis and increased activity of liver transaminases;
• damage to the hematopoietic organs: thrombocyto-, leuko- or neutropenia, megaloblastic anemia and agranulocytosis;
• symptoms associated with the urinary system: crystalluria, polyuria, hematuria, tubulointerstitial nephritis, increased urea levels, hypercreatininemia, renal dysfunction and toxic nephropathy (accompanied by anuria and oliguria);
• problems with the functioning of the musculoskeletal system: myalgia or arthralgia;
• signs of allergy: TEN, rashes, MEE (also includes SJS), photosensitivity, itching, myocarditis of allergic origin, exfoliative dermatitis, hyperemia affecting the sclera, Quincke's edema and increased temperature.

Overdose

Signs of poisoning: nausea, intestinal colic and vomiting, drowsiness, dizziness, depression, cephalgia, confusion and fainting; in addition, crystalluria, hematuria, visual disturbances and fever. With prolonged intoxication, jaundice, leukopenia, thrombocytopenia or megaloblastic anemia develop.

Gastric lavage and urine acidification (increases excretion of trimethoprim) are required, and oral fluid and Ca folinate are taken at 5-15 mg per day (eliminates the effect of trimethoprim on bone marrow). If necessary, hemodialysis is performed.

Interactions with other drugs

The drug increases the anticoagulant effect of indirect anticoagulants, methotrexate and antidiabetic drugs.

Biseptrim reduces the severity of intrahepatic metabolic processes of phenytoin (prolongs its half-life by 39%), as well as warfarin, potentiating their effect.

The drug reduces the reliability of oral contraceptives (suppresses intestinal microflora and reduces intestinal-hepatic circulation of hormonal elements).

Pyrimethamine in doses greater than 25 mg per week increases the likelihood of developing megaloblastic anemia.

Rifampicin reduces the half-life of trimethoprim.

Diuretics (mainly thiazides) increase the likelihood of thrombocytopenia.

The therapeutic effect of the drug is weakened when combined with procaine, benzocaine, procainamide, the hydrolysis of which forms PABA.

Cross-allergy may occur between orally administered antidiabetic agents (sulfonylurea derivatives) and diuretics (furosemide, thiazides, etc.) on the one hand, and antimicrobial sulfonamides on the other.

PAS and barbiturates with phenytoin potentiate the symptoms of vitamin B9 deficiency.

Salicylic acid derivatives potentiate the activity of Biseptrim.

Urine acidifiers hexamethylenetetramine and vitamin C increase the likelihood of crystalluria.

Cholestyramine weakens absorption, which is why it is used 4-6 hours before or 1 hour after the administration of co-trimoxazole.

Medicines that suppress bone marrow hematopoiesis increase the likelihood of myelosuppression.

Storage conditions

Biseptrim should be stored in a place inaccessible to small children. Temperature level – no more than 25°C.

Shelf life

Biseptrim can be used for a period of 36 months from the date of sale of the medicinal product.

Analogues

Analogues of the drug are Biseptol, Sumetrolim with Bi-sept, Groseptol, Baktiseptol and Oriprim.